5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Article Details
- CitationCopy to clipboard
Lewis TA, Bayless L, DiPesa AJ, Eckman JB, Gillard M, Libertine L, Scannell RT, Wypij DM, Young MA
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Bioorg Med Chem Lett. 2005 Feb 15;15(4):1083-5.
- PubMed ID
- 15686917 [ View in PubMed]
- Abstract
A series of N-hydroxycarbamates containing a histaminergic H(1) receptor antagonist pharmacophore was synthesized. In vitro assays determined the compounds had both histaminergic binding and 5-lipoxygenase inhibiting activities comparable to the corresponding N-hydroxyurea analog. Animal models demonstrated antihistaminergic and the 5-lipopxygenase inhibitory activity, with the N-hydroxyurea analog having a better overall profile.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Cetirizine Histamine H1 receptor Ki (nM) 5.89 N/A N/A Details Zileuton Arachidonate 5-lipoxygenase IC 50 (nM) 873 N/A N/A Details Zileuton Arachidonate 5-lipoxygenase IC 50 (nM) 518 N/A N/A Details